HUP9900611A2 - 2,7-substituted octahydro-pyrrolo[1,2-a]pyrazine derivatives, pharmaceutical compositions containing them and intermediates for the preparation of the compounds - Google Patents
2,7-substituted octahydro-pyrrolo[1,2-a]pyrazine derivatives, pharmaceutical compositions containing them and intermediates for the preparation of the compoundsInfo
- Publication number
- HUP9900611A2 HUP9900611A2 HU9900611A HUP9900611A HUP9900611A2 HU P9900611 A2 HUP9900611 A2 HU P9900611A2 HU 9900611 A HU9900611 A HU 9900611A HU P9900611 A HUP9900611 A HU P9900611A HU P9900611 A2 HUP9900611 A2 HU P9900611A2
- Authority
- HU
- Hungary
- Prior art keywords
- atom
- carbon
- compounds
- alkyl
- phenyl
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Toxicology (AREA)
- Anesthesiology (AREA)
- Addiction (AREA)
- Ophthalmology & Optometry (AREA)
- Psychology (AREA)
- Otolaryngology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
A találmány tárgyát (I) általánős képletű vegyületek, az ezekettartalmazó gyógyszerkészítmények és a vegyületek előállításánakközbenső termékei képezik. Az (I) általánős képletben R1 jelentése fenil-, naftil-, benzőxazőlőnil-, indőlil-, indőlőnil-,benzimidazőlil-, kinőlil-, fűril-, benzőfűril-, tienil-, benzőtienil-,őxazőlil-, benzőxazőlilcsőpőrt; R2 jelentése hidrőgénatőm vagy 1-6 szénatőmős alkilcsőpőrt, R3 jelentése fenil-, piridinil-, pirimidinil-, pirazinil- vagypiridazi- nilcsőpőrt, R4 jelentése hidrőgénatőm vagy 1-6 szénatőmős alkilcsőpőrt, R5 jelentése hidrőgénatőm vagy 1-6 szénatőmős alkilcsőpőrt - ahőladőtt esetben az R1 és R3 csőpőrt mindegyike egymástól függetlenül,adőtt esetben 1-4 szűbsztitűenssel lehet helyettesített, melyszűbsztitűens lehet flűőr-, klór-, bróm- jódatőm, cianő-, nitrő-,tiőcianőcsőpőrt, -SR4, -SOR4, -SO2R4, -NHSO2R4 általánős képletű, 1-6szénatőmős alkőxi-, -NR4R5, -NR4COR5, -CONR4R5 általánős képletű,fenil-, -COR4, -COOR4 általánős képletű, 1-6 szénatőmős alkil-, 1-6halőgénatőmmal helyettesített, 1-6 szénatőmős alkil-, 3-6 szénatőmősciklőalkil- vagy triflűőr-metőxi-csőpőrt, X jelentése őxigén-,kénatőm, SO, SO2, NR4, C=O, CH(OH), CHR4, -O-C(=O)-, -C(=O)-O-, -N(R4)-C(=O)- vagy -C(=O)-N(-R4)- képletű, illetve általánős képletűcsőpőrt; m jelentése 0, 1 vagy 2; n jelentése 0, 1 vagy 2; A találmány szerinti vegyületekdőpaminreceptőr altípűsők, különösen a dőpamin D4 receptőr ligandűmai,és mint ilyenek, alkalmasak a dőpaminrendszerrel összefüggő betegségekkezelésére vagy megelőzésére. ŕThe subject of the invention are compounds of the general formula (I), pharmaceutical preparations containing them and intermediate products of the production of the compounds. In the general formula (I), R1 is phenyl, naphthyl, benzoxazolyl, indolyl, indolyl, benzimidazolyl, quinolyl, furyl, benzofuryl, thienyl, benzothienyl, oxazolyl, benzoxazolyl; R2 is a hydrogen atom or a 1-6 carbon atom, R3 is a phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl atom, R4 is a hydrogen atom or an 1-6 carbon atom, R5 is a hydrogen atom or an 1-6 carbon alkyl atom - in which case R1 and R3 can be independently replaced by 1-4 substituents, which substituents can be fluorine, chlorine, bromine, iodine atom, cyano, nitro, thiocyano, -SR4, -SOR4, -SO2R4, -NHSO2R4 , 1-6 carbon-substituted alkyl-, -NR4R5, -NR4COR5, -CONR4R5, phenyl-, -COR4, -COOR4, 1-6-carbon alkyl-, 1-6-halogen substituted, 1-6-carbon alkyl-, 3- 6-carbon cyclic alkyl or trifluoromethoxy, X is oxygen, sulfur atom, SO, SO2, NR4, C=O, CH(OH), CHR4, -O-C(=O)-, -C(=O)-O -, -N(R4)-C(=O)- or -C(=O)-N(-R4)- formula, or universal formula powder; m is 0, 1 or 2; n is 0, 1 or 2; The compounds according to the invention are dopamine receptor subtypes, especially dopamine D4 receptor ligands, and as such are suitable for the treatment or prevention of diseases related to the dopamine system. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US898895P | 1995-12-21 | 1995-12-21 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9900611A2 true HUP9900611A2 (en) | 1999-08-30 |
| HUP9900611A3 HUP9900611A3 (en) | 2000-09-28 |
Family
ID=21734893
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9900611A HUP9900611A3 (en) | 1995-12-21 | 1996-11-06 | 2,7-substituted octahydro-pyrrolo[1,2-a]pyrazine derivatives, pharmaceutical compositions containing them and intermediates for the preparation of the compounds |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US5714487A (en) |
| EP (1) | EP0874849B1 (en) |
| JP (1) | JP3204456B2 (en) |
| KR (1) | KR100286786B1 (en) |
| CN (1) | CN1061350C (en) |
| AR (1) | AR005102A1 (en) |
| AT (1) | ATE205846T1 (en) |
| AU (1) | AU704578B2 (en) |
| BR (1) | BR9612246A (en) |
| CA (1) | CA2240594C (en) |
| CO (1) | CO4480107A1 (en) |
| CZ (1) | CZ192998A3 (en) |
| DE (1) | DE69615404T2 (en) |
| DK (1) | DK0874849T3 (en) |
| ES (1) | ES2161377T3 (en) |
| GR (1) | GR3037060T3 (en) |
| GT (1) | GT199600101A (en) |
| HU (1) | HUP9900611A3 (en) |
| IL (1) | IL124453A0 (en) |
| MA (1) | MA26413A1 (en) |
| MX (1) | MX9805088A (en) |
| NO (1) | NO309936B1 (en) |
| NZ (1) | NZ320537A (en) |
| PE (1) | PE25998A1 (en) |
| PL (1) | PL327539A1 (en) |
| PT (1) | PT874849E (en) |
| RU (1) | RU2162470C2 (en) |
| SI (1) | SI0874849T1 (en) |
| TN (1) | TNSN96164A1 (en) |
| TR (1) | TR199801161T2 (en) |
| TW (1) | TW479058B (en) |
| WO (1) | WO1997023482A1 (en) |
| ZA (1) | ZA9610781B (en) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6281216B1 (en) * | 1998-02-09 | 2001-08-28 | Duphar International Research B.V. | 2-aminoquinoline derivatives having d4-agonistic activity |
| EP0982030A3 (en) * | 1998-08-17 | 2000-05-10 | Pfizer Products Inc. | 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands |
| JP2002536376A (en) * | 1999-02-05 | 2002-10-29 | ファルマシア・アンド・アップジョン・カンパニー | Method for producing (5R)-(methylamino) -5,6-dihydro-4H-imidazo [4,5,1-ij] -quinolin-2 (1H) -one |
| US7125903B1 (en) | 1999-09-14 | 2006-10-24 | Aventis Pharmaceuticals Inc. | Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists |
| EE200200134A (en) * | 1999-09-14 | 2003-04-15 | Aventis Pharmaceuticals Inc. | Benzisoxazolyl, pyridoisoxazolyl and benzthienylphenoxy derivatives acting as D4 receptor antagonists |
| US7253165B2 (en) | 1999-09-14 | 2007-08-07 | Aventis Pharmaceuticals Inc. | Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as D4 antagonists |
| US7091199B1 (en) | 1999-09-14 | 2006-08-15 | Aventis Pharmaceuticals Inc. | Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d4 antagonists |
| TW200801005A (en) * | 2005-08-15 | 2008-01-01 | Astrazeneca Ab | Acetylenic piperazines as metabotropic glutamate receptor antagonists |
| US7728031B2 (en) * | 2006-02-24 | 2010-06-01 | Abbott Laboratories | Octahydro-pyrrolo[3,4-b]pyrrole derivatives |
| WO2013049164A1 (en) * | 2011-09-29 | 2013-04-04 | Abbvie Inc. | SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS |
| KR102639990B1 (en) * | 2018-03-28 | 2024-02-27 | 신토고교 가부시키가이샤 | Electric lift device and roll press device with electric lift device |
| JP7460264B2 (en) * | 2018-09-04 | 2024-04-02 | コンティニューム・セラピューティクス・インコーポレイテッド | Muscarinic acetylcholine M1 receptor antagonists |
| US11752149B2 (en) | 2019-12-02 | 2023-09-12 | Pipeline Therapeutics, Inc. | Muscarinic acetylcholine M1 receptor antagonists |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4400511A (en) * | 1982-05-07 | 1983-08-23 | American Home Products Corporation | 2-Substituted octahydropyrrolo(1,2-A)-pyrazine-3-carboxylic acids |
| WO1990008148A1 (en) * | 1989-01-23 | 1990-07-26 | Pfizer Inc. | Bis-aza-bicyclic anxiolytic agents |
| US5122515A (en) * | 1990-06-19 | 1992-06-16 | Smith Ross C | Nutrient composition containing dipeptides and method for administering the same |
| JP3058945B2 (en) * | 1990-10-26 | 2000-07-04 | 三共株式会社 | N- (3,3-disubstituted acryloyl) piperazine derivatives |
| ES2133416T3 (en) * | 1992-10-23 | 1999-09-16 | Merck Sharp & Dohme | LIGANDS OF DOPAMINE RECEPTOR SUBTYPES. |
| EP0665840A1 (en) * | 1992-10-23 | 1995-08-09 | MERCK SHARP & DOHME LTD. | Dopamine receptor subtype ligands |
| EP0775118B1 (en) * | 1994-08-05 | 2003-06-04 | Pfizer Inc. | Benzimidazole derivatives having dopaminergic activity |
| AU681310B2 (en) * | 1994-09-30 | 1997-08-21 | Pfizer Inc. | 2,7-substituted octahydro-1h-pyrido{1,2-a}pyrazine derivatives |
-
1996
- 1996-11-06 DK DK96935226T patent/DK0874849T3/en active
- 1996-11-06 WO PCT/IB1996/001192 patent/WO1997023482A1/en not_active Application Discontinuation
- 1996-11-06 TR TR1998/01161T patent/TR199801161T2/en unknown
- 1996-11-06 IL IL12445396A patent/IL124453A0/en unknown
- 1996-11-06 SI SI9630343T patent/SI0874849T1/xx unknown
- 1996-11-06 ES ES96935226T patent/ES2161377T3/en not_active Expired - Lifetime
- 1996-11-06 HU HU9900611A patent/HUP9900611A3/en unknown
- 1996-11-06 RU RU98111742/04A patent/RU2162470C2/en not_active IP Right Cessation
- 1996-11-06 EP EP96935226A patent/EP0874849B1/en not_active Expired - Lifetime
- 1996-11-06 PT PT96935226T patent/PT874849E/en unknown
- 1996-11-06 AT AT96935226T patent/ATE205846T1/en not_active IP Right Cessation
- 1996-11-06 PL PL96327539A patent/PL327539A1/en unknown
- 1996-11-06 CN CN96199250A patent/CN1061350C/en not_active Expired - Fee Related
- 1996-11-06 CA CA002240594A patent/CA2240594C/en not_active Expired - Fee Related
- 1996-11-06 NZ NZ320537A patent/NZ320537A/en unknown
- 1996-11-06 DE DE69615404T patent/DE69615404T2/en not_active Expired - Fee Related
- 1996-11-06 BR BR9612246A patent/BR9612246A/en not_active Application Discontinuation
- 1996-11-06 CZ CZ981929A patent/CZ192998A3/en unknown
- 1996-11-06 AU AU73280/96A patent/AU704578B2/en not_active Ceased
- 1996-11-06 JP JP52344697A patent/JP3204456B2/en not_active Expired - Fee Related
- 1996-11-06 KR KR1019980704718A patent/KR100286786B1/en not_active IP Right Cessation
- 1996-11-08 TW TW085113669A patent/TW479058B/en not_active IP Right Cessation
- 1996-12-16 AR ARP960105715A patent/AR005102A1/en not_active Application Discontinuation
- 1996-12-16 PE PE1996000913A patent/PE25998A1/en not_active Application Discontinuation
- 1996-12-18 MA MA24432A patent/MA26413A1/en unknown
- 1996-12-18 TN TNTNSN96164A patent/TNSN96164A1/en unknown
- 1996-12-19 GT GT199600101A patent/GT199600101A/en unknown
- 1996-12-20 ZA ZA9610781A patent/ZA9610781B/en unknown
- 1996-12-20 CO CO96066997A patent/CO4480107A1/en unknown
- 1996-12-23 US US08/774,290 patent/US5714487A/en not_active Expired - Fee Related
-
1998
- 1998-06-19 NO NO982843A patent/NO309936B1/en unknown
- 1998-06-22 MX MX9805088A patent/MX9805088A/en unknown
-
2001
- 2001-10-30 GR GR20010401932T patent/GR3037060T3/en not_active IP Right Cessation
Also Published As
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